G-protein-coupled receptors (GPCRs) have been tractable drug targets for decades with
over one-third of currently marketed drugs targeting GPCRs. Of these, the class A GPCR …

A comprehensive guide to privileged structures and their application in the discovery of new
drugs The use of privileged structures is a viable strategy in the discovery of new medicines …

A series of 4-substituted 2-amino-3-benzoylthiophenes was screened using a functional
assay of A1AR-mediated phosphorylation of ERK1/2 in intact CHO cells to identify both …

Despite intense interest in designing positive allosteric modulators (PAMs) as selective
drugs of the adenosine A1 receptor (A1AR), structural binding modes of the receptor PAMs …

Adenosine is a purine nucleoside, responsible for the regulation of a wide range of
physiological and pathophysiological conditions by binding with four G-protein-coupled …

Intense efforts of many pharmaceutical companies and academicians in the A 1 adenosine
receptor (AR) field have led to the discovery of clinical candidates that are antagonists …

G protein-coupled receptors (GPCRs) represent the target for approximately a third of FDA-
approved small molecule drugs. The adenosine A1 receptor (A1R), one of four adenosine …

Interest in adenosine deaminase (ADA) in the context of medicine has mainly focused on its
enzymatic activity. This is justified by the importance of the reaction catalyzed by ADA not …

Pain represents an international burden and a major socio-economic public health problem.
New findings, detailed in this review, suggest that adenosine plays a significant role in …

Allosteric receptor ligands bind to a recognition site that is distinct from the binding site of the
endogenous messenger molecule. As a consequence, allosteric agents may attach to …